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Heterocyclic Drugs from Plants
Published in Rohit Dutt, Anil K. Sharma, Raj K. Keservani, Vandana Garg, Promising Drug Molecules of Natural Origin, 2020
Debasish Bandyopadhyay, Valeria Garcia, Felipe Gonzalez
The root of Scutellaria baicalensis was studied and the root showed great potential as a neuroprotector. This plant did not execute any toxicity towards humans so far. The two major flavones that were isolated and characterized from the plant Scutellaria baicalensis are known as baicalein and oroxylin (Gasiorowski et al., 2011). These flavones have demonstrated cognitive and amnestic functions on the animals being studied for aging and degeneration of the brain. Baicalein is a flavone that has shown to aid the inhibition of neuronal amyloidogenic proteins and also helps out to induce the amyloid deposit. Additionally, baicalein is known to function as an anti-inflammatory, an anxiolytic, and takes away action of mild sedative agents. This plant also contains wogonin, a minor flavone constituent, having the potential to aid in brain tissue regeneration (Gasiorowski et al., 2011).
Herbs with Antidepressant Effects
Published in Scott Mendelson, Herbal Treatment of Major Depression, 2019
Scutellaria baicalensis is an ingredient in at least two of the most commonly used Traditional Chinese Medicine herbal combinations for the treatment of MDD, i.e., tiao qi and chai hu jia long gu mu li. Data do show that skullcap ameliorates many pathophysiologies that lead to depression, including systemic inflammation, Metabolic Syndrome, insulin resistance, chronic stress, and artificial elevation of corticosterone levels. These effects are also seen in the brain when animals are treated with specific phytochemical components of Scutellaria baicalensis, including baicalin, chrysin, and apigenin. Oroxylin A, a scutellaria flavonoid, stimulates neurogenesis in mouse hippocampus, which is yet another effect associated with antidepressant action.12 There is also a report that plants of this genus contain hyperforin, the primary antidepressant component of well-studied St John’s wort.13 Interestingly, flavonoids from Scutellaria lateriflora displace LSD from the 5-HT7 receptors, which is believed to play a role in MDD. It should be noted that the flavonoids responsible for this effect appear to bind with rather low high micromolar affinity and it is questionable if this has clinical significance.14
Abies Spectabilis (D. Don) G. Don (Syn. A. Webbiana Lindl.) Family: Coniferae
Published in L.D. Kapoor, Handbook of Ayurvedic Medicinal Plants, 2017
Ethanolic extract of stem bark on fractionation yielded oroxylin A, baicalein. scutellarein, and scutellarein-7-rutinoside, in different solvent extractives. Chrysin and baicalein-7-glucu-ronide and p-coumaric acid were also isolated from the mother liquor.675 Benzene extract of heartwood of O. indica yielded β-sitosterol and prunetin-4′, 5-dihydroxy-7-methoxyisoflavone.676
Application of the Mannich reaction in the structural modification of natural products
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Miao-Xia Pu, Hong-Yan Guo, Zhe-Shan Quan, Xiaoting Li, Qing-Kun Shen
Oroxylin A, a flavonoid from the Indian herb Oroxylum indicum, is a potent inhibitor. Babu et al.87 designed and synthesised a series of 8-aminomethylated derivatives based on oroxylin A with a methoxy group at the 6th position through the Mannich reaction and evaluated their effects on rat intestinal and yeast α-glucosidase inhibitory activities. The synthesised compounds significantly enhanced the a-glucosidase-inhibitory activity of the lead compounds (Table 4). Among them, compound 67 (Figure 5) with N-methyl piperazine at the C8 position showed the strongest inhibitory activity, with IC50 values of 35.43 and 98.84 µg/mL for rat intestinal a-glucosidase and yeast a-glucosidase, respectively. Regarding the structural features of the active Mannich bases, the results indicate that the 5,7-dihydroxy-6-methoxy groups on the A-ring of the flavonoid are the basis of glucosidase inhibition activity. Alicyclic amine substituents significantly improved the intestinal a-glucosidase inhibitory potential of the parent compound. Among them, the N-methylpiperazinyl substitution had the strongest inhibitory effect. This experiment showed that the introduction of alicyclic amines into natural compounds can significantly improve their activity, providing a direction for the results of natural products.
Metabolites identification and species comparison of Oroxylin A, an anti-cancer flavonoid, in vitro and in vivo by HPLC-Q-TOF-MS/MS
Published in Xenobiotica, 2022
Yueying Bian, Mengqi Sun, Huili Chen, Guanghui Ren, Kejia Fu, Nan Yang, Mei Zhang, Nan Zhou, Yang Lu, Ning Li, Yongjie Zhang, Xijing Chen, Di Zhao
Oroxylin A (OA, C16H12O5; Figure 1(A)) is one of the main components of the dry root of Scutellaria baicalensis Georigi, which was extracted first from the root bark of Bignonia indica Linnaeus (Lu et al. 2016). As a traditional Chinese medicine component, OA has antitumor activities through multiple pathways. Zhao et al. (2020) proved that OA triggered apoptosis through caspase-8 activation and p62/SQSTM1 proteolysis in hepatocellular carcinoma with dose of 64 μM, and Sun et al. (2019) showed that 20 μM OA could inhibit the growth of MDA-MB-231 through inactivating NF-κB signalling pathway. Otherwise, OA also has other properties such as anti-inflammatory (Shen et al. 2020) and treatment of nervous system diseases (Ji et al. 2020), which attracted the attention of many researchers for its potential to be developed as a novel drug.
The metabolic effect of gut microbiota on drugs
Published in Drug Metabolism Reviews, 2020
Yuan Xie, Fangdi Hu, Dawei Xiang, Hui Lu, Wenbin Li, Anpeng Zhao, Longji Huang, Rong Wang
Baicalin is the main active ingredient of the root of Scutellaria baicalensis. A large number of studies have indicated that it has antibacterial, anti-inflammatory, and anti-infection and other pharmacological effects. Trinh et al. (2010) found that the metabolites of baicalin by human intestinal flora were mainly deglycosylated baicalein and methylated aglycone oroxylin A, and the two metabolites’ effect on ameliorating histamine-induced pruritic reactions in mice were stronger than baicalin. In Magnus test using guinea pig ileum, oroxylin A is more potent than baicalein in inhibition of histamine-induced contraction (Trinh et al. 2010).